CHINESE JOURNAL OF CHEMISTRY
·
2016
·Vol. 34
·期 6
·609-616
·
IF 1.872
Wei Zhang,Wenjun Zhu,Ruiyu He,Shuo Fang,Yemin Zhang,Chen Yao,Muhammad Ismail,Xinsong Li
Chlorambucil is a classic nitrogen mustard drug that has been used in the treatment of cancers. It may induce neutropenia, thrombocytopenia and other side effects because of its short lifetime and off-target effect. In this report, chlorambucil-tetrapeptide (AAAK, A 3 K) conjugate vesicles were developed to improve the stability and bioactivity of chlorambucil. First of all, chlorambucil-A 3 K conjugate was synthesized by solid phase synthesis strategy. Secondly, the chlorambucil-A 3 K conjugate was assembled and characterized by critical aggregation concentration, circular dichroism, dynamic light scattering and transmission electron microscopy. The results indicated that the chlorambucil-A 3 K conjugate can be assembled to form spherical vesicles with an average diameter of 390.5 nm, and high drug loading about 47.1% is reached. Surprisingly, the preliminary biological evaluation of the chlorambucil-A 3 K conjugate vesicles revealed the best in vitro anticancer activity against HeLa, HepG-2 and MCF-7 cell lines compared with chlorambucil and chlorambucil-A 3 K conjugate free drugs. Furthermore, conjugate vesicles showed excellent in vivo antitumoral activity. It can be partly attributed to their vesicular structure which isolates chlorambucil active moiety from aqueous solution to retard degradation before killing cancer cells. Therefore, chlorambucil-peptide (A 3 K) conjugate vesicles may be an alternative delivery system of chlorambucil.
研究领域:
药学
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癌症研究
·
纳米技术
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
CHINESE JOURNAL OF ANALYTICAL CHEMISTRY
·
2021
·
IF 1.134
Xing WEI,Jing-Jing ZHOU,Jin-Hui LIU,Ming-Li CHEN,Jian-Hua WANG
Chromium plays an irreplaceable role in the life system. The exploration of chromium is beneficial to reveal its physiological or pathological processes. In this study, a novel method was established for determination of chromium in gels by matrix-matched external standard method-laser ablation inductively coupled plasma mass spectrometry (LA-ICP-MS). The relative standard deviation of chromium signal intensity during ablation standard were less than 16% ( n = 300), the correlation coefficient ( R 2 ) of LA-ICP-MS quantitative calibration curve was 0.9805, and the detection limit was 2.22 µg/g. The MCF-7 cells were used as an in vitro cell model, and two kinds of polyacrylamide gel electrophoresis (PAGE) method were used to separate the protein extract after chromium incubation. And then, the electrophoresis bands obtained by two electrophoresis methods were ablated respectively by LA-ICP-MS with line scan mode, and the weak chromium-containing protein bands were obtained in electrophoresis band. Finally, the LA-ICP-MS was used to measure and image the chromium in individual cell, and it was found that the cell element distribution map overlapped well with the cell contour map under the laser microscope.
研究领域:
分析化学
·
生物医学
✓ 已验证
产品关联
DOI
高影响因子
Journal of Materials Chemistry B
·
2015
·Vol. 3
·期 8
·1556-1564
·
IF 4.726
Xu Li,Cuixia Gao,Yupei Wu,C.-Yan Cheng,Weiliang Xia,Zhiping Zhang
Combination therapy has been regarded as a potent strategy to overcome multidrug resistance (MDR). In this study, we adopt Adjudin (ADD), a mitochondria inhibitor, and Doxorubicin (DOX), a common chemo-drug, to treat drug-resistant cancer cells (MCF-7/ADR) in combination. Given the different physico-chemical properties of ADD and DOX, we develop a novel drug formulation (ADD–DOX (M)) by integrating drug conjugation and nanocarrier approaches to realize the co-delivery of the two drugs. We demonstrate the conjugation of ADD and DOX via formation of an acid-sensitive hydrazone bond, and then the encapsulation of ADD–DOX conjugates by DSPE-PEG2000 micelles with high drug encapsulation efficiency and well-controllable drug loading efficiency. The obtained ADD–DOX (M) micelles are found to be stable under physiological conditions, but can rapidly release drugs within acidic environments. Following cellular experiments confirm that ADD–DOX (M) vehicles can be internalized by MCF-7/ADR cancer cells through an endocytic pathway and exist within the moderate acidic endolysosomes, thus accelerating the hydrolysis of ADD–DOX and the release of free ADD and DOX. As a result, the ADD–DOX (M) formulation exhibits an excellent anti-MDR effect. In summary, we for the first time report the combinational use of ADD and DOX with an effective co-delivery strategy for the treatment of MDR cancer cells.
研究领域:
药理学
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肿瘤学
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纳米技术
·
化疗
✓ 已验证
DOI
PubMed
高影响因子
Results in Chemistry
·
2025
·
IF 4.2
Basharat Ali,Muhammad Riaz,Ajmal Khan,Nadir Rasheed,Muhammad Masood,Ali Iftikhar,Amir Faisal,Sobia Ahsan Halim,Jalal Uddin,Afnan Jan,Ahmed Al-Harrasi
Carbothioamides exhibit many biological properties, including antiviral, antibacterial and anticancer activities. Their ability to interfere with DNA synthesis is mainly responsible for their anticancer activities. Here, twelve phenyl-substituted carbothioamides ( 2−13 ) were synthesized and characterized using Electron Ionization Mass Spectrometry (EI-MS), proton and carbon-13 nuclear magnetic resonance ((Singhal et al., 2013 [ 1 ] ) HNMR, and 13 C NMR), Infrared (IR), and elemental analysis. The anticancer activity of the carbothioamide derivatives ( 2–13 ) was measured in the HCT116 colorectal cancer cell line by means of a three day sulforhodamine B (SRB) proliferation assay. Among the series, four compounds ( 2 , 4 , 11 , and 12 ) which inhibited the cell viability by more than 50 % at 50 μM concentration. IC 50 determination of these four compounds revealed 1-benzoyl-4-(2-bromophenyl) thiosemicarbazide ( 11 ) as the most potent compound with IC 50 values of 21.61 ± 4.77 μM, 18.34 ± 3.53 μM and 17.87 ± 12.02 μM in the breast cancer (MCF-7) cell line, human colorectal carcinoma (HCT116) cell line and MD Anderson-metastatic breast (MDA-MB-453) cell lines respectively. Prolonged treatment of cells with the compound resulted in apoptotic cell death as determined by cleavage of Poly (ADP-ribose) polymerase (PARP), a caspase 3 substrate and an apoptotic marker. This study, therefore, explored novel derivatives of carbothioamides for their anticancer activities; the structure activity relationship (SAR) reported in this study and predicted docking analysis and ADMET profile will help optimize carbothioamides as anticancer agents.
研究领域:
药物化学
·
药理学
·
肿瘤学
·
生物化学
·
分子生物学
✓ 已验证
产品关联
DOI
高影响因子
International Journal of Nanomedicine
·
2017
·
IF 4.3
Ying Li,Meng Wang,Bu-Wei Huang,Yuan Ping,Jian You,Jian-Qing Gao
Although widely used in chemotherapy, free doxorubicin (Dox) might enhance cell malignancy undesirably. Liposomal Dox (Doxlipo) has been clinically approved for the treatment of breast cancer due to reduced systematical toxicity and increased tumor targeting, yet the transcriptome-wide elucidation of the Doxlipo formulations remains elusive. To this end, we explored the impact of two Dox liposomal formulations, Doxlipo mainly containing hydrogenated soy phosphatidylcholine or 1,2-dipalmitoyl-sn-glycero-3-phosphocholine, on the transcriptional pattern of MCF-7 cells. The two types of Dox liposomal formulations with different drug release kinetics were investigated to reveal the relationship between the formulation and tumor malignancy. Interestingly, we found that liposomal formulation significantly altered the transcriptional pattern of a wide range of genes. Under equivalent dosage of Dox, free Dox substantially changed the expression of ANK1, ACTA2, GPR87, GDF15, FZD6, and WNT4 in MCF-7 cells. Notably, free Dox induced much higher expression of ABCB1 and significantly enhanced the cell migration behavior in comparison with HSPC Doxlipo under a similar level of cytotoxicity. Finally, siRNA targeting GPR87 was codelivered with cationic Doxlipo to reduce the expression of malignancy-related genes. Our study, for the first time, provides an overview of the influence of formulation on the malignancy at transcriptional level and reveals the relationship between cytotoxicity and cell malignancy from the formulation aspect, offering valuable reference for the future formulation design for anticancer drug delivery.
研究领域:
药理学
·
肿瘤学
·
分子生物学
·
药物递送系统
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Scientific Reports
·
2017
·Vol. 7
·期 1
·1-12
·
IF 4.259
Song Chen,Wang Leyu,Ye Genlan,Song Xiaoping,He Yutong,Qiu Xiaozhong
Ammonium persulfate (APS), a low molecular weight chemical compound with strong oxidizing properties, should to be totally removed during preparation of nanomaterials due to its cytotoxicity. APS exerts its oxidative stress effects mainly on cell membrane, but its intracellular influence remains unclear. Here, we designed a facile negatively-charged carboxylic gelatin-methyacrylate (carbox-GelMA) nanoparticle (NP) as a cargo-carrier through the catalytic and oxidizing action of APS in W/O system. The formed APS-loaded carbox-GelMA NPs (APS/NPs) were transported into the lysosome in MCF-7 breast cancer cells. The intracellular APS/NPs produced a high level of oxidative stress in lysosome and induced epithelial-mesenchymal transition (EMT). Consequently, the MCF-7 cells challenged with APS/NPs had a strong metastatic and invasive capability in vitro and in vivo . This study highlights that a facile APS-loaded nanocarrier has cyctotoxicity on cells through EMT. Unexpectedly, we found a novel pathway inducing EMT via lysosomal oxidative stress.
研究领域:
纳米技术
·
细胞生物学
·
癌症研究
·
毒理学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF ELECTROANALYTICAL CHEMISTRY
·
2020
·
IF 3.807
Anzi Yang,Xiaoxia Huangfu,Lixiao Liu,Wen Luo,Wenbo Zhao,Jun Yin
Biomedical detection needs to develop more detection methods and reagents. CuFeS 2 , an I-III-IV ternary semiconductor material, has attracted great interest of researchers because of its optical, electrical, low toxicity and controllable chemical synthesis. Here, we synthesized CuFeS 2 quantum dots (QDs) with hot-injection method and their ECL behaviors were investigated for the first time, involving the co-reactant anode/cathode ECL emission and the related ECL mechanism. Moreover, a novel ECL immunosensor based on CuFeS 2 QDs for the ultrasensitive detection of Cyclin D1 (CCND1) was designed and prepared. CuFeS 2 QDs with uniform size and excellent optical properties were used as ECL emitters and Carboxyl Fe 3 O 4 magnetic beads (MB) were utilized for magnetic separation of CCND1 from MCF-7 cells treated by sophora frevescens. In addition, reduced graphene oxide (rGO) and Au NPs by electrodeposition not only provided plentiful active sites for the immobilization of anti-CCND1 (primary antibody, Ab 1 ), but also enhanced the conductivity of the electrode. Results indicated that under the optimal condition, the ECL signal was proportional to the logarithmic of CCND1 concentration in the linear range from 40 fg/mL to 0.8 μg/mL with a detection limit of 15.8 fg/mL. Further, the good reproducibility, stability and selectivity of the as-prepared ECL immunosensor were also proved. Significantly, the anticancer effect of sophora frevescens on MCF-7 cells was investigated through quantitative analysis of overexpression of CCND1, which was related to proliferation of cancer cells. This research indicated the ECL immunosensor we suggested could offer great potential for the follow-up research in clinical diagnosis and anticancer drug screening.
研究领域:
生物医学工程
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分析化学
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材料科学
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肿瘤学
✓ 已验证
产品关联
DOI
高影响因子
OPTICAL MATERIALS
·
2019
·
IF 2.687
Chunmei Huang,Ying Qian
For highly sensitive and selective detection of ClO − over other reactive oxygen species (ROS) and anions, a fluorescent probe MN-BODIPY by introducing a morpholine group into the 8-position of BODIPY which could be used for targeting lysosome and improving water solubility was designed and synthesized. As a result of the C=N isomerization mechanism at 2-position of BODIPY, the probe alone generated extremely weak fluorescence. However, in the presence of ClO − , the probe exhibited a dramatic enhancement of fluorescence intensity by a 29-fold increase at 530 nm accompanying with quantum yield changing from 0.03 to 0.25. Accordingly, the probe displayed fast response for ClO − within 60 s. The limit of detection (LOD) for ClO − was calculated as 16.5 nM from the titration experiments, which is lower than most previously reported ClO − -selective probes. Moreover, MN-BODIPY had been successfully employed for monitoring exogenous and endogenous hypochlorous in MCF-7 cells with satisfying results, perhaps it was feasible for detecting abnormal contents of hypochlorous in a biological system and accomplished the goal of maintaining normal human activities. At last, the fluorescence imaging showed that MN-BODIPY was capable of localizing lysosomes in living cells.
研究领域:
分析化学
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生物化学
·
细胞生物学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY
·
2017
·Vol. 17
·期 5
·2873-2880
·
IF 1.483
Huang Saiyan,Liu Jieying,Zhu Hao,Hussain Abid,Liu Qing,Li Jing,Shen Yuanyuan,Cheng Jiejun,Guo Shengrong
A novel folate-polyethylene glycol-succinic acid-doxorubicin conjugate (FA-PEG-SA-DOX) micelle loaded with curcumin (CUR) is designed and prepared to target tumor cells via folate-folate receptor interactions and co-deliver chemotherapeutic agent DOX and chemosensitizer CUR for treatment
of multidrug resistant human breast cancer MCF-7/ADR cells. The CUR/FA-PEG-SA-DOX micelles are characterized with the average size of 90.64±0.15 nm and the zeta potential of −15.3±0.8 mV. The CUR and DOX contents of the micelles are 12.07 and 15.69% (w/w), respectively.
The cytotoxicity, cellular uptake and effiux of the micelles are investigated by using MCF-7/ADR cells. The results demonstrate that the CUR/FA-PEG-SA-DOX micelles have greater toxicity (IC50 = 3.10 µg/ml) compared to the free DOX (IC50 = 31.99 µg/ml),
moreover, the micelles present increased cellular uptake and reduced cellular effiux. The combination index of CUR/FA-PEG-SA-DOX micelles was 0.17, which indicate a strong synergistic antitumor efficacy against MCF-7/ADR cells. These results suggest that Curcumin-loaded FA-PEG-SA-DOX micelles
may be a promising nanomedicine for co-delivery dual-drug treatment for cancer.
研究领域:
药学
·
肿瘤学
·
纳米技术
·
药物递送系统
✓ 已验证
产品关联
DOI
高影响因子
Journal of Innovative Optical Health Sciences
·
2022
·
IF 2.396
Xiao Ma,Honglian Xiong,Jinhao Guo,Zhiming Liu,Yaru Han,Mingdi Liu,Yanxian Guo,Mingyi Wang,Huiqing Zhong,Zhouyi Guo
Because the breast cancer is an important factor that threatens women’s lives and health, early diagnosis is helpful for disease screening and a good prognosis. Exosomes are nanovesicles, secreted from cells and other body fluids, which can reflect the genetic and phenotypic status of parental cells. Compared with other methods for early diagnosis of cancer (such as circulating tumor cells (CTCs) and circulating tumor DNA), exosomes have a richer number and stronger biological stability, and have great potential in early diagnosis. Thus, it has been proposed as promising biomarkers for diagnosis of early-stage cancer. However, distinguishing different exosomes remain is a major biomedical challenge. In this paper, we used predictive Convolutional Neural model to detect and analyze exosomes of normal and cancer cells with surface-enhanced Raman scattering (SERS). As a result, it can be seen from the SERS spectra that the exosomes of MCF-7, MDA-MB-231 and MCF-10A cells have similar peaks (939, 1145 and 1380 cm − 1 ). Based on this dataset, the predictive model can achieve 95% accuracy. Compared with principal component analysis (PCA), the trained CNN can classify exosomes from different breast cancer cells with a superior performance. The results indicate that using the sensitivity of Raman detection and exosomes stable presence in the incubation period of cancer cells, SERS detection combined with CNN screening may be used for the early diagnosis of breast cancer in the future.
研究领域:
癌症生物学
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生物医学工程
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医学诊断
·
机器学习
✓ 已验证
产品关联
DOI
高影响因子
COLLOIDS AND SURFACES B-BIOINTERFACES
·
2023
·
IF 5.8
Jidong Wang,Yating Zhang,Min Dong,Zhaopeng Liu,Binbin Guo,Haipeng Zhang,Liming Gao
Detecting and analyzing circulating tumor cells(CTCs) is significant for early diagnosis, management, and personalized treatment of tumors. Herein, a smart magnetic aptamer modified Fe 3 O 4 @ZIF-8 core/shell structured nanoparticle (NPs) was successfully constructed using for capture and simultaneous pH- and NIR-irradiation responsive release of CTCs. Taking MCF-7 as model CTCs, it could be captured ca. 60 % in low-concentration artificial blood by aptamer (SYL3C) on the surface of Fe 3 O 4 @ZIF-8 NPs. After magnetic separation, the ZIF-8 shell in aptamer-modified Fe 3 O 4 @ZIF-8 NPs carrying captured CTCs would disintegrate within 20 min under the synergistic effect of an acidic environment (pH=6.0) and NIR irradiation leading to the release of CTCs with high cell viability , which was benefited for the subsequent culture and analysis. This magnetic and core/shell structured device integrated high-efficiency capture, quick isolation and perfect release into one system, which showed great potential s for the detection of CTCs in the clinic.
研究领域:
生物医学工程
·
纳米技术
·
癌症诊断
·
细胞生物学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
JOURNAL OF MATERIALS SCIENCE
·
2020
·Vol. 55
·期 29
·14530-14543
·
IF 3.553
Qi Zeer,Shi Jun,Zhu Beibei,Li Jingguo,Cao Shaokui
Abstract In this paper, a novel one-pot strategy was utilized to immobilize gold nanorods (GNRs) onto the surface of PEGylated graphene oxide (GO-PEG) via polydopamine (PDA) to fabricate GNRs/GO@PDA hybrid nanosheets. The GNRs/GO@PDA nanosheets possessed excellent photostability and photothermal conversion efficiency (36.10%), due to the robust interfacial immobilization of PDA between GNRs and GO-PEG. Besides, GNRs/GO@PDA also could be utilized to be an efficient drug nano-vehicle that possessed an excellent loading ability for anticancer drug doxorubicin hydrochloride (DOX) (86.16%). Furthermore, the drug release of hybrid nanosheets could be triggered by pH value and near-infrared (NIR) light irradiation, which could be mainly ascribed to the strong π – π stacking interaction between GNRs/GO@PDA and DOX, as well as the brilliant NIR-responsive property of GNRs/GO@PDA. It was found that GNRs/GO@PDA possessed extremely low cytotoxicity to MCF-7 cells even at 250 μg mL −1 , while GNRs/GO@PDA(DOX) showed obvious cytotoxicity at 100 μg mL −1 . Thus, this paper presents a feasible strategy to fabricate GNRs/GO hybrid nanosheets with high drug loading capacity, excellent photothermal conversion property and pH/NIR-stimuli-responsive drug delivery performance, which possesses brilliant potentials to be an efficient platform for remotely triggered drug delivery. Graphical abstract
研究领域:
纳米技术
·
生物医学工程
·
药学
·
材料科学
✓ 已验证
产品关联
DOI
高影响因子
危险品化学品经营许可证（带存储）